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WO2002008244A3 - Peptides as ns3-serine protease inhibitors of hepatitis c virus - Google Patents

Peptides as ns3-serine protease inhibitors of hepatitis c virus Download PDF

Info

Publication number
WO2002008244A3
WO2002008244A3 PCT/US2001/022678 US0122678W WO0208244A3 WO 2002008244 A3 WO2002008244 A3 WO 2002008244A3 US 0122678 W US0122678 W US 0122678W WO 0208244 A3 WO0208244 A3 WO 0208244A3
Authority
WO
WIPO (PCT)
Prior art keywords
hepatitis
peptides
virus
protease inhibitors
serine protease
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2001/022678
Other languages
French (fr)
Other versions
WO2002008244A2 (en
Inventor
Anil K Saksena
Viyyoor Moopil Girijavallabhan
Raymond G Lovey
Edwin E Jao
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Dendreon Pharmaceuticals LLC
Original Assignee
Schering Corp
Corvas International Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22822095&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2002008244(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to DE60141608T priority Critical patent/DE60141608D1/en
Priority to HU0401730A priority patent/HU229997B1/en
Priority to NZ523782A priority patent/NZ523782A/en
Priority to EP01954764A priority patent/EP1385870B1/en
Priority to AT01954764T priority patent/ATE461207T1/en
Priority to MXPA03000627A priority patent/MXPA03000627A/en
Priority to JP2002514149A priority patent/JP4298289B2/en
Priority to SI200130967T priority patent/SI1385870T1/en
Priority to CA2410662A priority patent/CA2410662C/en
Application filed by Schering Corp, Corvas International Inc filed Critical Schering Corp
Priority to AU2001276988A priority patent/AU2001276988B2/en
Priority to SK75-2003A priority patent/SK288064B6/en
Priority to HK04100762.2A priority patent/HK1058047B/en
Priority to IL15367001A priority patent/IL153670A0/en
Priority to KR1020037000784A priority patent/KR100904788B1/en
Priority to AU7698801A priority patent/AU7698801A/en
Priority to DK01954764.5T priority patent/DK1385870T3/en
Priority to BR0112540-0A priority patent/BR0112540A/en
Publication of WO2002008244A2 publication Critical patent/WO2002008244A2/en
Priority to IL153670A priority patent/IL153670A/en
Priority to NO20030272A priority patent/NO332329B1/en
Anticipated expiration legal-status Critical
Publication of WO2002008244A3 publication Critical patent/WO2002008244A3/en
Priority to LU91910C priority patent/LU91910I2/en
Priority to CY2011020C priority patent/CY2011020I2/en
Priority to DE201212000004 priority patent/DE122012000004I1/en
Priority to NO2013003C priority patent/NO2013003I2/en
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
PCT/US2001/022678 2000-07-21 2001-07-19 Peptides as ns3-serine protease inhibitors of hepatitis c virus Ceased WO2002008244A2 (en)

Priority Applications (23)

Application Number Priority Date Filing Date Title
BR0112540-0A BR0112540A (en) 2000-07-21 2001-07-19 Peptides as Hepatitis C Virus Ns-3-Serine Protease Inhibitors
HK04100762.2A HK1058047B (en) 2000-07-21 2001-07-19 Peptides as ns3-serine protease inhibitors of hepatitis c virus
NZ523782A NZ523782A (en) 2000-07-21 2001-07-19 Peptides as NS3-serine protease inhibitors of hepatitis C virus
EP01954764A EP1385870B1 (en) 2000-07-21 2001-07-19 Peptides as ns3-serine protease inhibitors of hepatitis c virus
KR1020037000784A KR100904788B1 (en) 2000-07-21 2001-07-19 Novel Peptides as Hepatic C Virus Inhibitors of Ns3-serine Protease
MXPA03000627A MXPA03000627A (en) 2000-07-21 2001-07-19 Novel peptides as ns3-serine protease inhibitors of hepatitis c virus.
JP2002514149A JP4298289B2 (en) 2000-07-21 2001-07-19 Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
SI200130967T SI1385870T1 (en) 2000-07-21 2001-07-19 Peptides as ns3-serine protease inhibitors of hepatitis c virus
CA2410662A CA2410662C (en) 2000-07-21 2001-07-19 Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
HU0401730A HU229997B1 (en) 2000-07-21 2001-07-19 Peptides as ns3-serine protease inhibitors of hepatitis c virus
AU2001276988A AU2001276988B2 (en) 2000-07-21 2001-07-19 Peptides as NS3-serine protease inhibitors of hepatitis C virus
SK75-2003A SK288064B6 (en) 2000-07-21 2001-07-19 Peptide compounds, pharmaceutical compositions comprising them and their use
IL15367001A IL153670A0 (en) 2000-07-21 2001-07-19 Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
DE60141608T DE60141608D1 (en) 2000-07-21 2001-07-19 PEPTIDES AS INHIBITORS OF THE NS3 SERINE PROTEASE OF HEPATITIS C VIRUS
AT01954764T ATE461207T1 (en) 2000-07-21 2001-07-19 PEPTIDES AS INHIBITORS OF THE NS3 SERINE PROTEASE OF THE HEPATITIS C VIRUS
AU7698801A AU7698801A (en) 2000-07-21 2001-07-19 Novel peptides as NS3-serine protease inhibitors of hepatitis c virus
DK01954764.5T DK1385870T3 (en) 2000-07-21 2001-07-19 Peptides as inhibitors of NS3 serine protease from hepatitis C virus
IL153670A IL153670A (en) 2000-07-21 2002-12-25 Peptides as ns3-serine protease inhibitors of hepatitis c virus
NO20030272A NO332329B1 (en) 2000-07-21 2003-01-20 Compounds such as NS3 serine protease inhibitors for hepatitis C virus, pharmaceutical preparations and use of the compounds for the manufacture of a drug.
LU91910C LU91910I2 (en) 2000-07-21 2011-12-02 Boceprevir - Victrelis
CY2011020C CY2011020I2 (en) 2000-07-21 2011-12-16 NOVEL PEPTIDES AS NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS
DE201212000004 DE122012000004I1 (en) 2000-07-21 2012-01-13 Peptides as inhibitors of the hepatitis C virus NS3 serine protease.
NO2013003C NO2013003I2 (en) 2000-07-21 2013-02-12 Compounds as NS3 serine protease inhibitors for hepatitis C virus, pharmaceutical preparations and use of the compounds in the manufacture of a medicament

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22010800P 2000-07-21 2000-07-21
US60/220,108 2000-07-21

Publications (2)

Publication Number Publication Date
WO2002008244A2 WO2002008244A2 (en) 2002-01-31
WO2002008244A3 true WO2002008244A3 (en) 2003-06-19

Family

ID=22822095

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/022678 Ceased WO2002008244A2 (en) 2000-07-21 2001-07-19 Peptides as ns3-serine protease inhibitors of hepatitis c virus

Country Status (31)

Country Link
US (4) US7012066B2 (en)
EP (1) EP1385870B1 (en)
JP (3) JP4298289B2 (en)
KR (2) KR100904788B1 (en)
CN (3) CN1498224A (en)
AR (2) AR033985A1 (en)
AT (1) ATE461207T1 (en)
AU (2) AU2001276988B2 (en)
BR (1) BR0112540A (en)
CA (1) CA2410662C (en)
CY (2) CY1112267T1 (en)
CZ (1) CZ303213B6 (en)
DE (2) DE60141608D1 (en)
DK (1) DK1385870T3 (en)
EC (1) ECSP034438A (en)
ES (1) ES2341534T3 (en)
HU (1) HU229997B1 (en)
IL (2) IL153670A0 (en)
LU (1) LU91910I2 (en)
MX (1) MXPA03000627A (en)
MY (2) MY143322A (en)
NO (2) NO332329B1 (en)
NZ (1) NZ523782A (en)
PL (1) PL206255B1 (en)
PT (1) PT1385870E (en)
RU (2) RU2355700C9 (en)
SI (1) SI1385870T1 (en)
SK (1) SK288064B6 (en)
TW (1) TWI324611B (en)
WO (1) WO2002008244A2 (en)
ZA (1) ZA200210312B (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7378422B2 (en) 2003-09-05 2008-05-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US7427681B2 (en) 2000-12-21 2008-09-23 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7528142B2 (en) 2005-11-03 2009-05-05 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
US7557106B2 (en) 2002-06-20 2009-07-07 Vertex Pharmaceuticals Incorporated Substituted pyrimidines useful as protein kinase inhibitors
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
US11851422B2 (en) 2021-07-09 2023-12-26 Aligos Therapeutics, Inc. Anti-viral compounds

Families Citing this family (267)

* Cited by examiner, † Cited by third party
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EP0932617B1 (en) 1996-10-18 2002-01-16 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
PE20011350A1 (en) 2000-05-19 2002-01-15 Vertex Pharma PROPHARMAC OF AN INHIBITOR OF INTERLEUKIN-1ß CONVERTER ENZYME (ICE)
IL153670A0 (en) * 2000-07-21 2003-07-06 Schering Corp Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
US7244721B2 (en) * 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
SV2003000617A (en) 2000-08-31 2003-01-13 Lilly Co Eli INHIBITORS OF PROTEASA PEPTIDOMIMETICA REF. X-14912M
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
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MXPA04003825A (en) 2001-10-24 2004-07-08 Vertex Pharma Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system.
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US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US7273885B2 (en) * 2002-04-11 2007-09-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
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